555553

Rho Kinase Inhibitor III, Rockout

The Rho Kinase Inhibitor III, Rockout, also referenced under CAS 7272-84-6, controls the biological activity of Rho Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : Rho Kinase Inhibitor III, Rockout, 3-(4-Pyridyl)-1H-indole
• Formule empirique (notation de Hill) : C₁₃H₁₀N₂
• CAS Number: 7272-84-6
• Poids moléculaire : 194.23
• Numéro MDL: MFCD01035958
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.54

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: DMSO: 25 mg/mL; methanol: soluble
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• Chaîne SMILES: [nH]1c2c(c(c1)c3ccncc3)cccc2

Description

Description générale

A cell-permeable indolopyridine compound that acts as a selective, reversible, and ATP-competitive inhibitor of Rho kinase activity with an IC₅₀ of 25 µM. Does not inhibit the activation of Rho kinase nor does it affect the in vitro activities of MLCK, PKCα, and SAPK2a/p38α. Shown to be 5-fold less potent than Y-27632 (Cat. No. 688000; IC₅₀ = ~5 µM), and display a similar specificity profile as H-89 (Cat. No. 371963). Affects cell migration, inhibits blebbing (IC₅₀ = ~ 12 µM in M2 cells), and decreases stress fibers in Bulb 3T3 cells at 50 µM.

A cell-permeable, selective, reversible, and ATP-competitive inhibitor of Rho kinase activity (IC₅₀ = 25 µM). Does not inhibit the activation of Rho kinase nor does it affect the in vitro activities of MLCK, PKCα, and SAPK2a/p38α. Shown to be 5-fold less potent than Y-27632 (Cat. No. 688000; IC₅₀ ~5 µM), and display a similar specificity profile as H-89 (Cat. No. 371963). Affects cell migration, inhibits blebbing (IC₅₀ ~12 µM in M2 cells), and decreases stress fibers in Bulb 3T3 cells at 50 µM.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
ROCK

Product competes with ATP.

Reversible: yes

Target IC₅₀: 25 µM against ROCK

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Yarrow, J.C., et al. 2005. Chem. Biol.12, 385.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1